Results 41 to 50 of about 4,858 (185)

N-terminal BET bromodomain inhibitors disrupt a BRD4-p65 interaction and reduce inducible nitric oxide synthase transcription in pancreatic β-cells

Frontiers in Endocrinology, 2022
Chronic inflammation of pancreatic islets is a key driver of β-cell damage that can lead to autoreactivity and the eventual onset of autoimmune diabetes (T1D).
Joshua A. Nord, Sarah L. Wynia-Smith, Alyssa L. Gehant, Rachel A. Jones Lipinski, Aaron Naatz, Inmaculada Rioja, Rab K. Prinjha, John A. Corbett, Brian C. Smith   +8 more
doaj   +1 more source

Bromodomain: an acetyl‐lysine binding domain [PDF]

FEBS Letters, 2002
Bromodomains, an extensive family of evolutionarily conserved protein modules originally found in proteins associated with chromatin and in nearly all nuclear histone acetyltransferases, have been recently discovered to function as acetyl‐lysine binding domains.
Zeng, Lei, Zhou, Ming-Ming
openaire   +2 more sources

Discovery of SKP2‐Recruiting PROTACs for Target Protein Degradation

Advanced Science, EarlyView.
Based on the SKP2‐targeting ligand SL1, we designed non‐covalent PROTACs by linking it with the BRD4 inhibitor JQ1 and the AR antagonist AL through a linker. These PROTACs successfully induced the ubiquitination of BRD4 and AR, followed by proteasome‐mediated degradation.
Guanjun Dong, Aima Huang, Ziqing Zhao, Bikai Lai, Xin Pan, Huiyu Yang, Xiaohan Xu, Tianwei Wang, Fangchen Zhao, Zhimin Zhang, Yongbo Xue, Guanjun Deng, Wenbin Deng, Jianwei Chen   +13 more
wiley   +1 more source

Targeting Lactate and Lactylation in Cancer Metabolism and Immunotherapy

Advanced Science, EarlyView.
Lactate, once deemed a metabolic waste, emerges as a central regulator of cancer progression. This review elucidates how lactate and its epigenetic derivative, protein lactylation, orchestrate tumor metabolism, immune suppression, and therapeutic resistance.
Jiajing Gong, Yuhang Xie, Zhijie Weng, Yongzhi Wu, Longjiang Li, Bo Li   +5 more
wiley   +1 more source

OTUD6A in Airway Epithelial Cells Exacerbates Allergic Asthma by Promoting Airway Inflammation and Airway Remodeling Through Deubiquitination of hResistin/mRELMα

Advanced Science, EarlyView.
This study elucidates a novel mechanistic role of the deubiquitinase OTUD6A in asthma pathogenesis, uncovering its regulatory function in airway inflammation and airway remodeling through the stabilization of hResistin/mRELMα. This study offers a novel regulatory axis (OTUD6A‐hResistin/mRELMα) in asthma pathogenesis and OTUD6A inhibition as a potential
Weiting Pan, Xinru Xi, Wei Dai, Tingfang Xiao, Yeqing Chen, Xuanyu Chen, Xiangting Ge, Chengguang Zhao, Hui Zhang, Yali Zhang, Weixi Zhang   +10 more
wiley   +1 more source

The Development and Evaluation of a Novel Highly Selective PET Radiotracer for Targeting BET BD1

Pharmaceuticals
Background/Objectives: Small molecules that interfere with the interaction between acetylated protein tails and the tandem bromodomains of BET (bromodomain and extra-terminal) family proteins are pivotal in modulating immune/inflammatory and neoplastic ...
Yanli Wang, Yongle Wang, Yulong Xu, Leyi Kang, Darcy Tocci, Changning Wang   +5 more
doaj   +1 more source

Dihydropyridine Lactam Analogs Targeting BET Bromodomains

ChemMedChem, 2021
AbstractInhibitors of Bromodomain and Extra Terminal (BET) proteins are investigated for various therapeutic indications, but selectivity for BRD2, BRD3, BRD4, BRDT and their respective tandem bromodomains BD1 and BD2 remains suboptimal. Here we report selectivity‐focused structural modifications of previously reported dihydropyridine lactam 6 by ...
Jiewei Jiang, Logan H. Sigua, Alice Chan, Prakriti Kalra, William C.K. Pomerantz, Ernst Schönbrunn, Jun Qi, Gunda I. Georg   +7 more
openaire   +4 more sources

Identification of A p300–SP1–BRD4 Transcriptional Axis as a Key Driver of AR Hyperactivation in Polycystic Ovarian Syndrome

Advanced Science, EarlyView.
This study reveals a pivotal epigenetic regulatory role for the histone acetyltransferase p300, demonstrating that its acetylation of histone 3 at lysine 18 and 27 (H3K18ac and H3K27ac), alongside the formation of the p300/BRD4/SP1 complex, drives AR activation and ovarian fibrosis in PCOS.
Zhengquan Zhu, Yihan Wang, Haiyun Chen, Xinye Yu, Tingyu Wang, Yajing Weng, Meihong Guo, Ying Huang, Gaojian Tao, Wangsen Cao, Yong Wang, Daojuan Wang   +11 more
wiley   +1 more source

Segmental Isotope Labelling of an Individual Bromodomain of a Tandem Domain BRD4 Using Sortase A.

PLoS ONE, 2016
Bromodomain and extra-terminal (BET) family of proteins are one of the major readers of epigenetic marks and an important target class in oncology and other disease areas. The importance of the BET family of proteins is manifested by the explosion in the
Felix P Williams, Alexander G Milbradt, Kevin J Embrey, Romel Bobby   +3 more
doaj   +1 more source

Cellular Identity Crisis: RD3 Loss Fuels Plasticity and Immune Silence in Progressive Neuroblastoma

Advanced Science, EarlyView.
Researchers discovered that therapy‐induced loss of RD3 protein in neuroblastoma triggers a dangerous shift: cancer cells become more stem‐like, invasive, and resistant to treatment while evading immune detection. RD3 loss suppresses antigen presentation and boosts immune checkpoints, creating an immune‐silent environment.
Poorvi Subramanian, Sreenidhi Mohanvelu, Sheeja Aravindan, Afsana Parveen Jahir Hussain, Sivasubramani Narayanan, Sabir Salim, Loganayaki Periyasamy, Natarajan Aravindan   +7 more
wiley   +1 more source